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Pronunciation:

(METH i leen bloo)

U.S. Brand Names:

Urolene Blue®

Generic Available:

Yes

Use:

Antidote for cyanide poisoning and drug-induced methemoglobinemia, indicator dye

Use - Unlabeled/Investigational:

Has been used topically (0.1% solutions) in conjunction with polychromatic light to photoinactivate viruses such as herpes simplex; has been used alone or in combination with vitamin C for the management of chronic urolithiasis

Pregnancy Risk Factor:

C/D (injected intra-amniotically)

Contraindications:

Hypersensitivity to methylene blue or any component of the formulation; intraspinal injection; renal insufficiency; pregnancy (injected intra-amniotically)

Warnings/Precautions:

Do not inject SubQ or intrathecally; use with caution in young patients and in patients with G6PD deficiency; continued use can cause profound anemia

Adverse Reactions:

Frequency not defined.

Cardiovascular: Hypertension, precordial pain

Central nervous system: Dizziness, mental confusion, headache, fever

Dermatologic: Staining of skin

Gastrointestinal: Fecal discoloration (blue-green), nausea, vomiting, abdominal pain

Genitourinary: Discoloration of urine (blue-green), bladder irritation

Hematologic: Anemia

Miscellaneous: Diaphoresis

Overdosage/Toxicology:

Symptoms of overdose include nausea, vomiting, precordial pain, hypertension, methemoglobinemia, cyanosis; overdosage has resulted in methemoglobinemia and cyanosis

Treatment is symptomatic and supportive

Mechanism of Action:

Weak germicide in low concentrations, hastens the conversion of methemoglobin to hemoglobin; has opposite effect at high concentrations by converting ferrous ion of reduced hemoglobin to ferric ion to form methemoglobin; in cyanide toxicity, it combines with cyanide to form cyanmethemoglobin preventing the interference of cyanide with the cytochrome system

Pharmacodynamics/Kinetics:

Absorption: Oral: 53% to 97%

Excretion: Urine and feces

Dosage:

Children: NADPH-methemoglobin reductase deficiency: Oral: 1-1.5 mg/kg/day (maximum: 300 mg/day) given with 5-8 mg/kg/day of ascorbic acid

Children and Adults: Methemoglobinemia: I.V.: 1-2 mg/kg or 25-50 mg/m² over several minutes; may be repeated in 1 hour if necessary

Adults: Genitourinary antiseptic: Oral: 65-130 mg 3 times/day with a full glass of water (maximum: 390 mg/day)

Administration:

Administer I.V. undiluted by direct I.V. injection over several minutes.

Patient Education:

May discolor urine and feces blue-green; take oral formulation after meals with a glass of water; skin stains may be removed using a hypochlorite solution

Additional Information:

Skin stains may be removed using a hypochlorite solution.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Dosage Forms:

Injection, solution: 10 mg/mL (1 mL, 10 mL)

Tablet (Urolene Blue®): 65 mg

References

Burnakis TG, "Inadvertent Substitution of Methylene Blue for Indigo Carmine to Detect Premature Rupture of Membranes,"Hosp Pharm, 1995, 30(4):336-8.

Dawson AH and Whyte IM, "Management of Dapsone Poisoning Complicated by Methaemoglobinaemia,"Med Toxicol Adverse Drug Exp, 1989, 4(5):387-92.

DiSanto AR and Wagner JG, "Pharmacokinetics of Highly Ionized Drugs II: Methylene Blue - Absorption, Metabolism, and Excretion in Man and Dog After Oral Administration,"J Pharm Sci, 1972, 61(7):1086-90.

Harvey JW and Keitt AS, "Studies of the Efficacy and Potential Hazards of Methylene Blue Therapy in Aniline-Induced Methaemoglobinaemia,"Br J Haematol, 1983, 54(1):29-41.

Jahns BE, Rynn KO, and Paloucek FP, "Interference of Methylene Blue (MthB) in the Determination of Whole Blood Methemoglobin (MtHgb) Concentrations,"Vet Hum Toxicol, 1994, 36:342.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings,"Chest, 2003, 123(3):897-922.

Preiser JC, Lejeune P, Roman A, et al, "Methylene Blue Administration in Septic Shock: A Clinical Trial,"Crit Care Med, 1995, 23(2):259-64.

Zulian GB, Tullen E, and Maton B, "Methylene Blue for Ifosfamide-Associated Encephalopathy,"N Engl J Med, 1995, 332(18):1239-40.

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